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1. 发明授权

US06596726B1 Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family 失效
标题翻译：能抑制表皮生长因子受体家族酪氨酸激酶的三环化合物
公开(公告)号：US06596726B1
公开(公告)日：2003-07-22
申请号：US08811803
申请日：1997-03-06
申请人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson , Howard Daniel Hollis Showalter
发明人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson , Howard Daniel Hollis Showalter
IPC分类号： A61K31505
CPC分类号： C07D471/04 , C07D239/70 , C07D471/14 , C07D473/34 , C07D487/04 , C07D491/04 , C07D491/14 , C07D495/04 , C07D513/04 , C07D513/14
摘要： Described are compounds of the following formula and a method of inhibiting epidermal growth factor by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of the formula: wherein the formula terms are described in the specification and wherein the members in the aforementioned structure are defined in the specification.
摘要翻译：描述了下式的化合物和抑制表皮生长因子的方法：通过以有效抑制量治疗有需要的哺乳动物，下式的化合物：其中式术语在说明书中描述，其中成员上述结构在说明书中定义。

2. 发明授权

US06713484B2 Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family 失效
标题翻译：能够抑制表皮生长因子受体家族酪氨酸激酶的双环化合物
公开(公告)号：US06713484B2
公开(公告)日：2004-03-30
申请号：US10201808
申请日：2002-07-24
申请人： Alexander James Bridges , William Alexander Denny , David Fry , Gordon William Rewcastle
发明人： Alexander James Bridges , William Alexander Denny , David Fry , Gordon William Rewcastle
IPC分类号： A61K31519
CPC分类号： C07D471/04 , A61K31/4985 , A61K31/519 , C07D473/34 , C07D495/04
摘要： Described are heterocyclic pyrimidine derivatives and a method of inhibiting epidermal growth factor by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of the formula: where: at least two of A-E are nitrogen, with the remaining atom(s) carbon; X=NH or NR7, such that R7=lower alkyl (1-4 carbon atoms), OH, NH2, lower alkoxy (1-4 carbon atoms) or lower monoalkylamino (1-4 carbon atoms); n=0, 1, 2. The remaining substituents are described in detail in the specification.
摘要翻译：描述的是杂环嘧啶衍生物和抑制表皮生长因子的方法，其中：有效抑制量的哺乳动物，有需要的下列化合物：其中：至少两个AE是氮，剩余的原子（ s）碳; X = NH或NR 7，使得R 7 =低级烷基（1-4个碳原子），OH，NH 2，低级烷氧基（1-4个碳原子）或低级单烷基氨基（1-4 碳原子）; n = 0,1,2。其余取代基在说明书中详细描述。

3. 发明授权

US06521620B1 Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family 失效
标题翻译：能够抑制表皮生长因子受体家族酪氨酸激酶的双环化合物
公开(公告)号：US06521620B1
公开(公告)日：2003-02-18
申请号：US09183190
申请日：1998-10-30
申请人： Alexander James Bridges , William Alexander Denny , David Fry , Gordon William Rewcastle
发明人： Alexander James Bridges , William Alexander Denny , David Fry , Gordon William Rewcastle
IPC分类号： A61K314985
CPC分类号： C07D471/04 , A61K31/4985 , A61K31/519 , C07D473/34 , C07D495/04
摘要： Described are heterocyclic pyrimidine derivatives and a method of inhibiting epidermal growth factor by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of the formula: where: at least two of A-E are nitrogen, with the remaining atom(s) carbon; X=NH or NR7, such that R7=lower alkyl (1-4 carbon atoms), OH, NH2, lower alkoxy (1-4 carbon atoms) or lower monoalkylamino (1-4 carbon atoms); n=0, 1, 2. The remaining substituents are described in detail in the specification.
摘要翻译：描述的是杂环嘧啶衍生物和抑制表皮生长因子的方法，其中：有效抑制量的哺乳动物，有需要的下列化合物：其中：至少两个AE是氮，剩余的原子（ X = NH或NR7，使得R7 =低级烷基（1-4个碳原子），OH，NH2，低级烷氧基（1-4个碳原子）或低级单烷基氨基（1-4个碳原子）; n = 剩余的取代基在说明书中详细描述。

4. 发明授权

US5679683A Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family 失效
标题翻译：能抑制表皮生长因子受体家族酪氨酸激酶的三环化合物
公开(公告)号：US5679683A
公开(公告)日：1997-10-21
申请号：US358352
申请日：1994-12-23
申请人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson , Howard Daniel Hollis Showalter
发明人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson , Howard Daniel Hollis Showalter
IPC分类号： A61K31/519 , A61P15/00 , A61P35/00 , C07D213/00 , C07D239/00 , C07D239/70 , C07D333/00 , C07D471/04 , C07D471/14 , C07D473/34 , C07D487/04 , C07D491/04 , C07D491/14 , C07D495/04 , C07D498/14 , C07D513/04 , C07D513/14 , A61K31/505 , C07D487/00
CPC分类号： C07D471/04 , C07D239/70 , C07D471/14 , C07D473/34 , C07D487/04 , C07D491/04 , C07D491/14 , C07D495/04 , C07D513/04 , C07D513/14
摘要： Novel 4-substituted amino benzothieno�3,2-d!pyrimidine and 4-substituted amino�2,3-d!pyrimidine inhibitors of epidermal growth factor receptor family of tyrosine kinases are described, as well as pharmaceutical compositions of the same, which are useful in treating proliferative diseases such as cancer, synovial pannus invasion in arthritis, psoriasis, vascular restenosis and angiogenesis and additionally useful in the treatment of pancreatitis and kidney disease as well as a contraceptive agent.
摘要翻译：描述了新型4-取代氨基苯并噻吩并[3,2-d]嘧啶和酪氨酸激酶表皮生长因子受体家族的4-取代氨基[2,3-d]嘧啶抑制剂及其药物组合物，其中可用于治疗增生性疾病如癌症，关节炎中的滑膜血管us入侵，牛皮癣，血管再狭窄和血管发生，并且还可用于治疗胰腺炎和肾脏疾病以及避孕药。

5. 发明授权

US5654307A Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family 失效
标题翻译：能够抑制表皮生长因子受体家族酪氨酸激酶的双环化合物
公开(公告)号：US5654307A
公开(公告)日：1997-08-05
申请号：US358351
申请日：1994-12-23
申请人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson
发明人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson
IPC分类号： A61K31/519 , A61P15/00 , A61P35/00 , C07D213/00 , C07D239/00 , C07D239/70 , C07D333/00 , C07D471/04 , C07D471/14 , C07D473/34 , C07D487/04 , C07D491/04 , C07D491/14 , C07D495/04 , C07D498/14 , C07D513/04 , C07D513/14 , A61K31/505 , C07D487/00
CPC分类号： C07D471/04 , C07D239/70 , C07D471/14 , C07D473/34 , C07D487/04 , C07D491/04 , C07D491/14 , C07D495/04 , C07D513/04 , C07D513/14
摘要： Novel 4-substituted amino pyrido pyrimidine and 4-substituted amino pyrido pyrimidine inhibitors of epidermal growth factor receptor family of tyrosine kinase are described, as well as pharmaceutical compositions of the same, which are useful in treating proliferative diseases such as cancer, synovial pannus invasion in arthritis, psoriasis, vascular restenosis and angiogenesis and additionally useful in the treatment of pancreatitis and kidney disease as well as a contraceptive agent.
摘要翻译：本发明描述了新型4-取代氨基吡啶并嘧啶和酪氨酸激酶表皮生长因子受体家族的4-取代氨基吡啶并嘧啶抑制剂及其药物组合物，其可用于治疗增殖性疾病如癌症，滑膜血管us入侵在关节炎，牛皮癣，血管再狭窄和血管发生中，另外可用于治疗胰腺炎和肾脏疾病以及避孕药。

6. 发明授权

US06455534B2 Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family 失效
标题翻译：能够抑制表皮生长因子受体家族酪氨酸激酶的双环化合物
公开(公告)号：US06455534B2
公开(公告)日：2002-09-24
申请号：US09824606
申请日：2001-04-02
申请人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson
发明人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson
IPC分类号： A61K31519
CPC分类号： C07D471/04 , A61K31/4985 , A61K31/519 , C07D473/34 , C07D495/04
摘要： Described are compounds and a method of inhibiting epidermal growth factor receptor tyrosine kinase by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of Formula II: where: one of A or E is nitrogen, with remaining atoms carbon; X=O, S, NH or NR7, such that R7=lower alkyl (1-4 carbon atoms), OH, NH2, lower alkoxy (1-4 carbon atoms) or lower monoalkylamino (1-4 carbon atoms). Other terms are described in the specification.
摘要翻译：通过用有效抑制量治疗有需要的哺乳动物，描述了化合物和抑制表皮生长因子受体酪氨酸激酶的方法，其中：A或E中的一个是氮，其余的原子碳 ; X = O，S，NH或NR7，使得R7 =低级烷基（1-4个碳原子），OH，NH2，低级烷氧基（1-4个碳原子）或低级单烷基氨基（1-4个碳原子）。其他术语在说明书中描述。

7. 发明授权

US06265410B1 Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family 失效
标题翻译：能够抑制表皮生长因子受体家族酪氨酸激酶的双环化合物
公开(公告)号：US06265410B1
公开(公告)日：2001-07-24
申请号：US09191163
申请日：1998-11-13
申请人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson
发明人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson
IPC分类号： A61K31519
CPC分类号： C07D471/04 , A61K31/4985 , A61K31/519 , C07D473/34 , C07D495/04
摘要： Described are compositions and a method of inhibiting epidermal growth factor receptor tyrosine kinase by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of Formula II: where: any two continguous positions in positions A-E taken together can be a single heteroatom selected from the group consisting of nitrogen, oxygen or sulfur, in which case the other two remaining atoms must be carbon; the remaining substituents are disclosed in the specification
摘要翻译：描述了通过以有效抑制量治疗需要其的哺乳动物治疗式II化合物来抑制表皮生长因子受体酪氨酸激酶的组合物和方法：其中：一起位置AE中的任何两个相对位置可以是选自氮，氧或硫的单个杂原子，其中另外两个剩余的原子必须是碳; 剩余的取代基在说明书中公开

8. 发明授权

US6084095A Substituted pyrido[3,2-d]pyrimidines capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family 失效
标题翻译：能够抑制表皮生长因子受体家族酪氨酸激酶的取代的吡啶并[3,2-d]嘧啶
公开(公告)号：US6084095A
公开(公告)日：2000-07-04
申请号：US811797
申请日：1997-03-06
申请人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson
发明人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson
IPC分类号： C07D487/04 , A61K31/495 , A61K31/4985 , A61K31/505 , A61K31/519 , A61K31/525 , A61P1/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D239/00 , C07D471/04 , C07D471/14 , C07D473/34 , C07D487/02 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04
CPC分类号： C07D471/04 , A61K31/4985 , A61K31/519 , C07D473/34 , C07D495/04
摘要： Novel 4-substituted amino pyrido [3,2-d]pyrimidine inhibitors of epidermal growth factor receptor family of tyrosine kinases are described, as well as pharmaceutical compositions of the same, which are useful in treating proliferative diseases such as cancer, synovial pannus invasion in arthritis, psoriasis, vascular restenosis and angiogenesis and additionally useful in the treatment of pancreatitis and kidney disease as well as a contraceptive agent.
摘要翻译：本发明描述了新型的4-取代氨基吡啶并[3,2-d]嘧啶抑制剂，其酪氨酸激酶表皮生长因子受体家族及其药物组合物可用于治疗增殖性疾病如癌症，滑膜血管us入侵在关节炎，牛皮癣，血管再狭窄和血管发生中，另外可用于治疗胰腺炎和肾脏疾病以及避孕药。

9. 发明授权

US07169778B2 Pteridinones as kinase inhibitors 失效
标题翻译：蝶啶酮作为激酶抑制剂
公开(公告)号：US07169778B2
公开(公告)日：2007-01-30
申请号：US10070530
申请日：2000-06-21
申请人： William Alexander Denny , Gordon William Rewcastle , Ellen Dobrusin , James Bernard Kramer , Dennis Joseph McNamara , Howard Daniel Hollis Showalter , Peter Laurence Toogood
发明人： William Alexander Denny , Gordon William Rewcastle , Ellen Dobrusin , James Bernard Kramer , Dennis Joseph McNamara , Howard Daniel Hollis Showalter , Peter Laurence Toogood
IPC分类号： A61K31/535 , C07D475/00
CPC分类号： C07D475/00
摘要： Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4 and R6 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl; and R8 is hydrogen, lower alkyl or an (un)substituted carbocyclic group containing from 3–7 members, up to two of which members are optionally hetero atoms selected from oxygen and nitrogen; or R8 is (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl. These compounds are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The present invention also provides a method of treating cell proliferative disorders. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula (I).
摘要翻译：公开了式（Ia），（Ib），（Ic），（Id）的化合物，其中：W是NH，S，SO或SO 2; R 2是（未）取代的芳基，（未）取代的杂芳基或（取代的）取代的碳环或杂环; Q是氢或低级烷基; R 4和R 6相同或不同，表示氢，卤素，低级烷基，低级烷氧基，（未）取代的芳基，（未）取代的杂芳基，（un ）取代的芳基烷基或（未）取代的杂芳基烷基; 和R 8是氢，低级烷基或含有3-7个成员的（未）取代的碳环，其中至多两个成员任选是选自氧和氮的杂原子; 或（R 8）是（un）取代的芳基，（未）取代的杂芳基，（未）取代的芳基烷基或（未）取代的杂芳基烷基。这些化合物可用于治疗细胞增殖性疾病，如癌症和再狭窄。这些化合物是细胞周期蛋白依赖性激酶（cdks）和生长因子介导的激酶的有效抑制剂。本发明还提供了治疗细胞增殖性疾病的方法。本发明还提供含有式（I）化合物的药学上可接受的组合物。

10. 发明申请

US20110053907A1 SUBSTITUTED PYRIMIDINES AND TRIAZINES AND THEIR USE IN CANCER THERAPY 审中-公开
标题翻译：替代吡嘧啶和三氮唑及其在癌症治疗中的应用
公开(公告)号：US20110053907A1
公开(公告)日：2011-03-03
申请号：US12934616
申请日：2009-03-26
申请人： Gordon William Rewcastle , Peter Robin Shepherd , Glaire Chaussade , William Alexander Denny , Swarnalatha Akuratiya Gamage
发明人： Gordon William Rewcastle , Peter Robin Shepherd , Glaire Chaussade , William Alexander Denny , Swarnalatha Akuratiya Gamage
IPC分类号： A61K31/5377 , C07D413/14 , C07D401/14 , C07D487/04 , A61K31/53 , A61P35/00
CPC分类号： C07D251/18 , C07D401/12 , C07D403/12 , C07D487/04
摘要： Provided herein are substituted pyrimidine and triazine derivatives, including bicyclic pyrimidine derivatives, their pharmaceutical compositions, their preparation, and their use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. In one embodiment, the pyrimidine and triazine derivatives are morpholino-pyrimidine, morpholino-triazine, pyridyl-pyrimidine, and pyridyl-triazine derivatives which are selective irreversible inhibitors of the p110α isoform of PI3K.
摘要翻译：本文提供了取代的嘧啶和三嗪衍生物，包括双环嘧啶衍生物，它们的药物组合物，它们的制备及其用作癌症治疗的药物或药物，单独或与辐射和/或其它抗癌药物组合。在一个实施方案中，嘧啶和三嗪衍生物是作为PI3K的p110α同种型的选择性不可逆抑制剂的吗啉代 - 嘧啶，吗啉代 - 三嗪，吡啶基 - 嘧啶和吡啶基 - 三嗪衍生物。

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